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  • SPD304
SPD304的可视化放大

SPD304

A small-molecule inhibitor of TNFα activity

原价
¥687-7800
价格
550-6240
SPD304的二维码

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  • 货号: ajce50508
  • CAS: 869998-49-2
  • 别名:
  • 分子式: C32H32F3N3O2
  • 分子量: 547.61
  • 纯度: >98%
  • 溶解度: DMSO : 25 mg/mL (45.65 mM) Water : 20 mg/mL (36.52 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Tumor necrosis factor α (TNFα) is a primary mediator of many inflammatory conditions including rheumatoid arthritis, toxic shock, and sepsis.1,2,3 TNFα functions as a trimer and promotes receptor trimerization to activate proinflammatory and/or apoptotic signalling pathways. 4,5 SPD-304 is an inhibitor of tumor necrosis factor α (TNFα). that prevents binding to the TNF Receptor 1 (TNFR1) with an IC50 of 22 ?M.6 It binds to the biologically active TNFα trimer and promotes accelerated displacement of a single subunit to rapidly inactivate the cytokine. In a cell based assay, SPD-304 inhibited TNFα-mediated stimulation of IKB degradation with an IC50 of 4.6 ?M.6


1.Beutler, B., Greenwald, D., Hulmes, J.D., et al.Identity of tumor necrosis factor and the macrophage-secreted factor cachectinNature316552-554(1985) 2.Tracey, K.J., Beutler, B., Lowry, S.F., et al.Shock and tissue injury induced by recombinant human cachectinScience234470-474(1986) 3.Bidgood, M.J., Jamal, O.S., Cunningham, A.M., et al.Type IIA secretory phospholipase A2 up-regulates cyclooxygenase-2 and amplifies cytokine-mediated prostaglandin production in human rheumatoid synoviocytesJ. Immunol.1652790-2797(2000) 4.Thornberry, N.A., and Lazebnik, Y.Caspases: Enemies withinScience281(5381)1312-1316(1998) 5.Wallach, D., Varfolomeev, E.E., Malinin, N.L., et al.Tumor necrosis factor receptor and Fas signaling mechanismsAnnu. Rev. Immunol.17133-167(1999) 6.He, M.M., Smith, A.S., Oslob, J.D., et al.Small-molecule inhibition of TNF-αScience3101022-1025(2005)

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